Loxoprofen
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Also known as Loxoprofen acidLoxoprofeneLoxoprofenoSID50106490SID85231106SID90341428SID144203729SID170465808
Summary
Loxoprofen (CHEMBL19299) is an approved small-molecule non-steroidal anti-inflammatory drug (ATC M01AE19) targeting PTGS2; indicated across 8 conditions including rheumatic disorder and muscle tissue disorder.
At a glance
- Status: Approved (max clinical phase 4)
- Modality: Small molecule
- ATC class: M01AE19 (+1 more)
- Targets: 1 (PTGS2)
- Indications: 8 conditions
- Clinical trials: 13
- Chemistry: 246.3 Da · C15H18O3
Identifiers
Drug identity and classification
| Field | Value |
|---|---|
| ChEMBL ID | CHEMBL19299 |
| Name | Loxoprofen |
| Type | Small molecule |
| Max phase | 4 |
| FDA approved | no |
| PubChem CID | 3965 |
| ChEBI | CHEBI:76172 |
| ATC | M01AE19, M02AA31 |
| Molecular formula | C15H18O3 |
| Molecular weight | 246.3 |
| InChIKey | YMBXTVYHTMGZDW-UHFFFAOYSA-N |
SMILES: CC(C1=CC=C(C=C1)CC2CCCC2=O)C(=O)O
IUPAC name: 2-[4-[(2-oxocyclopentyl)methyl]phenyl]propanoic acid
ChEBI definition: A monocarboxylic acid that is propionic acid in which one of the hydrogens at position 2 is substituted by a 4-[(2-oxocyclopentyl)methyl]phenyl group. A prodrug that is rapidly converted into its active trans-alcohol metabolite following oral administration.
Pharmacological roles (ChEBI): non-steroidal anti-inflammatory drug, non-narcotic analgesic, antipyretic, EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor, prodrug.
Also known as: Loxoprofen, Loxoprofen acid, Loxoprofene, Loxoprofeno, loxoprofen, SID50106490, SID85231106, SID90341428, LOXOPROFENE, SID144203729, SID170465808, LOXOPROFEN
Parent form; salt/anhydrous children: CHEMBL66552
Patent coverage: 3,756 distinct patent families (13,531 SureChEMBL compound mentions), from 1 matched compound structure(s). Mentions count patents naming the compound (not distinct inventions), so promiscuous / reference molecules inflate the mention figure — families are the dedup metric.
Targets
Targets
Primary targets (GtoPdb curated mechanism): the Cancer dependency column is the DepMap CRISPR fitness signal (% of screened cell lines dependent on the target).
| Gene | Target | Action | pAffinity | Cancer dependency | UniProt |
|---|---|---|---|---|---|
| PTGS2 | COX-2 | Inhibition | 6.52 | 0% | P35354 |
Broader ChEMBL bioactivity targets: 6 (assay-derived). Sample: Endonuclease 4, Histone-lysine N-methyltransferase 2A, Prostaglandin G/H synthase 1, Prostaglandin G/H synthase 2, Kappa-type opioid receptor, Huntingtin.
Bioactivity
ChEMBL activities: 2 potent at pChembl ≥ 5 of 6 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):
| Target | pChembl | Type | Value | Unit | Activity ID |
|---|---|---|---|---|---|
| OPRK1 | 6.18 | AC50 | 660 | nM | CHEMBL_ACT_25129555 |
| PTGS1 | 5.19 | IC50 | 6500 | nM | CHEMBL_ACT_91899 |
Target pathways
Aggregated over 1 target gene(s): PTGS2.
Top Reactome pathways
8 total, by targets touching each:
| Pathway | Targets | Genes |
|---|---|---|
| Synthesis of 15-eicosatetraenoic acid derivatives | 1 | PTGS2 |
| Synthesis of Prostaglandins (PG) and Thromboxanes (TX) | 1 | PTGS2 |
| Interleukin-10 signaling | 1 | PTGS2 |
| Interleukin-4 and Interleukin-13 signaling | 1 | PTGS2 |
| Biosynthesis of DHA-derived SPMs | 1 | PTGS2 |
| Biosynthesis of EPA-derived SPMs | 1 | PTGS2 |
| Biosynthesis of DPAn-3 SPMs | 1 | PTGS2 |
| Biosynthesis of electrophilic ω-3 PUFA oxo-derivatives | 1 | PTGS2 |
Dominant GO biological processes
| GO term | Targets |
|---|---|
| prostaglandin biosynthetic process | 1 |
| response to oxidative stress | 1 |
| embryo implantation | 1 |
| regulation of blood pressure | 1 |
| response to nematode | 1 |
| response to selenium ion | 1 |
| positive regulation of vascular endothelial growth factor production | 1 |
| cyclooxygenase pathway | 1 |
| lipoxygenase pathway | 1 |
| positive regulation of prostaglandin biosynthetic process | 1 |
| positive regulation of fever generation | 1 |
| prostaglandin secretion | 1 |
| regulation of cell population proliferation | 1 |
| long-chain fatty acid biosynthetic process | 1 |
| positive regulation of nitric oxide biosynthetic process | 1 |
Indications & clinical
Indications
8 indications (3 at ChEMBL trial phase 4). Phase below is the highest clinical-trial phase recorded for this drug against each disease — not the molecule’s overall approval status (that is in the Summary).
| Indication | Trial phase | MONDO | EFO |
|---|---|---|---|
| rheumatic disorder | 4 | MONDO:0005554 | EFO:0005755 |
| muscle tissue disorder | 2 | MONDO:0003939 | EFO:0002970 |
| rheumatoid arthritis | 2 | MONDO:0008383 | EFO:0000685 |
5 further indication records had no mapped disease name (EFO/MeSH-only) or were duplicates, and are omitted.
Clinical trials
Total trials: 13.
Phase distribution
| Phase | Trials |
|---|---|
| PHASE2 | 4 |
| Not specified | 3 |
| PHASE4 | 2 |
| PHASE3 | 2 |
| PHASE1 | 2 |
Top trials by phase / activity
| NCT | Phase | Status | Title |
|---|---|---|---|
| NCT00994461 | PHASE4 | COMPLETED | Study Of Celecoxib In Healthy Subjects |
| NCT03800797 | PHASE4 | COMPLETED | Efficacy and Safety of Loxoprofen Hydrogel Patch in Patients With Ankylosing Spondylitis |
| NCT00141154 | PHASE3 | COMPLETED | Comparison Of Celecoxib 200 Mg Bid, Loxoprofen Sodium 60 Mg Tid And Placebo In Low Back Pain In Japan |
| NCT01779271 | PHASE3 | COMPLETED | Phase 3 Study of Pelubiprofen & Loxoprofen in Patients With Upper Respiratory Tract Infection |
| NCT01491321 | PHASE2 | UNKNOWN | Bee Venom Acupuncture for the Treatment of Chronic Low Back Pain |
| NCT01922466 | PHASE2 | COMPLETED | East-West Collaboration Treatment Using Bee Venom Acupuncture and NSAIDs for Chronic Cervicalgia |
| NCT02467504 | PHASE2 | COMPLETED | Low-dose Recombinant Human IL-2 for the Treatment of Rheumatoid Arthritis |
| NCT06047483 | PHASE2 | UNKNOWN | A Trial of HRF2105 Patch in Relieving Pain of Osteoarthritis |
| NCT06510413 | PHASE1 | NOT_YET_RECRUITING | An Bioequivalence Study of Loxoprofen Sodium Patches in Healthy Volunteers |
| NCT00676117 | PHASE1 | COMPLETED | Drug-Drug Interaction Study of Esomeprazole (D961H) Capsule and Loxoprofen Tablet After Repeated Oral Administration in Japanese Males |
| NCT07378059 | Not specified | RECRUITING | The Analgesic Efficacy and Safety of Loxoprofen Sodium Patch in Patients With Herpes Zoster |
| NCT07591207 | Not specified | NOT_YET_RECRUITING | The Efficacy and Safety of Loxoprofen Sodium Patch in Relieving Postoperative Pain After Laparoscopic Surgery |
| NCT07591220 | Not specified | NOT_YET_RECRUITING | The Efficacy and Safety of Loxoprofen Sodium Patch in Relieving Postoperative Pain After Thoracoscopic Surgery |
Clinical evidence (CIViC)
No CIViC predictive evidence (expected for non-precision-medicine drugs).
Pharmacology
Pharmacogenomics
No CPIC/DPWG dosing guideline, but PharmGKB curates 2 clinical and 2 variant annotation(s) for this drug (gene-keyed; see PharmGKB).
Related molecules
Related molecules
Molecules sharing ≥1 of this drug’s curated primary targets, merged from two biobtree sources and ranked by shared-target count, then clinical phase: ChEMBL clinical-stage candidates (development phase ≥2) and PubChem drug-class bioactivity (approved / known drugs acting on the target). Deduplicated by drug name; the drug’s own salt forms are excluded. Note: for a drug with few primary targets a shared-target match can reflect off-target / promiscuous binding rather than the same therapeutic mechanism — the phase ordering surfaces bona-fide therapeutics first.
201 molecules share ≥1 primary target. Top 60 by shared-target count:
| Molecule | Source | Status | Shared targets |
|---|---|---|---|
| FIDAXOMICIN | ChEMBL + PubChem | Phase 4 (approved) | PTGS2 |
| 3,3’,4’,5-TETRACHLOROSALICYLANILIDE | ChEMBL | Phase 4 (approved) | PTGS2 |
| ABEMACICLIB | ChEMBL | Phase 4 (approved) | PTGS2 |
| ACALABRUTINIB | ChEMBL | Phase 4 (approved) | PTGS2 |
| ACEMETACIN | ChEMBL | Phase 4 (approved) | PTGS2 |
| ACETOPHENAZINE | ChEMBL | Phase 4 (approved) | PTGS2 |
| ACETYLCYSTEINE | ChEMBL | Phase 4 (approved) | PTGS2 |
| ACRIVASTINE | ChEMBL | Phase 4 (approved) | PTGS2 |
| AMODIAQUINE | ChEMBL | Phase 4 (approved) | PTGS2 |
| AMPHOTERICIN B | ChEMBL | Phase 4 (approved) | PTGS2 |
| AMSACRINE | ChEMBL | Phase 4 (approved) | PTGS2 |
| ANISINDIONE | ChEMBL | Phase 4 (approved) | PTGS2 |
| APOMORPHINE | ChEMBL | Phase 4 (approved) | PTGS2 |
| ARFORMOTEROL | ChEMBL | Phase 4 (approved) | PTGS2 |
| ASPIRIN | ChEMBL | Phase 4 (approved) | PTGS2 |
| BAZEDOXIFENE | ChEMBL | Phase 4 (approved) | PTGS2 |
| BENZQUINAMIDE | ChEMBL | Phase 4 (approved) | PTGS2 |
| BEPRIDIL | ChEMBL | Phase 4 (approved) | PTGS2 |
| BIPERIDEN | ChEMBL | Phase 4 (approved) | PTGS2 |
| BROMFENAC | ChEMBL | Phase 4 (approved) | PTGS2 |
| CALCIPOTRIENE | ChEMBL | Phase 4 (approved) | PTGS2 |
| CALCITRIOL | ChEMBL | Phase 4 (approved) | PTGS2 |
| CANDESARTAN CILEXETIL | ChEMBL | Phase 4 (approved) | PTGS2 |
| CANNABIDIOL | ChEMBL | Phase 4 (approved) | PTGS2 |
| CAPSAICIN | ChEMBL | Phase 4 (approved) | PTGS2 |
| CAPTOPRIL | ChEMBL | Phase 4 (approved) | PTGS2 |
| CARPROFEN | ChEMBL | Phase 4 (approved) | PTGS2 |
| CEFAZOLIN | ChEMBL | Phase 4 (approved) | PTGS2 |
| CEFTIZOXIME | ChEMBL | Phase 4 (approved) | PTGS2 |
| CELECOXIB | ChEMBL | Phase 4 (approved) | PTGS2 |
| CEPHRADINE | ChEMBL | Phase 4 (approved) | PTGS2 |
| CIANIDANOL | ChEMBL | Phase 4 (approved) | PTGS2 |
| CLOTRIMAZOLE | ChEMBL | Phase 4 (approved) | PTGS2 |
| CRIZOTINIB | ChEMBL | Phase 4 (approved) | PTGS2 |
| DAUNORUBICIN | ChEMBL | Phase 4 (approved) | PTGS2 |
| DESERPIDINE | ChEMBL | Phase 4 (approved) | PTGS2 |
| DEXIBUPROFEN | ChEMBL | Phase 4 (approved) | PTGS2 |
| DEXKETOPROFEN | ChEMBL | Phase 4 (approved) | PTGS2 |
| DICLOFENAC | ChEMBL | Phase 4 (approved) | PTGS2 |
| DIETHYLSTILBESTROL | ChEMBL | Phase 4 (approved) | PTGS2 |
| DOBUTAMINE | ChEMBL | Phase 4 (approved) | PTGS2 |
| DOXORUBICIN | ChEMBL | Phase 4 (approved) | PTGS2 |
| EPINEPHRINE | ChEMBL | Phase 4 (approved) | PTGS2 |
| ERGOTAMINE | ChEMBL | Phase 4 (approved) | PTGS2 |
| ESFLURBIPROFEN | ChEMBL | Phase 4 (approved) | PTGS2 |
| ETODOLAC | ChEMBL | Phase 4 (approved) | PTGS2 |
| ETORICOXIB | ChEMBL | Phase 4 (approved) | PTGS2 |
| FLUPIRTINE | ChEMBL | Phase 4 (approved) | PTGS2 |
| FLURBIPROFEN | ChEMBL | Phase 4 (approved) | PTGS2 |
| FLUVASTATIN | ChEMBL | Phase 4 (approved) | PTGS2 |
| FOLIC ACID | ChEMBL | Phase 4 (approved) | PTGS2 |
| GLAFENINE | ChEMBL | Phase 4 (approved) | PTGS2 |
| HALOPERIDOL | ChEMBL | Phase 4 (approved) | PTGS2 |
| HEXACHLOROPHENE | ChEMBL | Phase 4 (approved) | PTGS2 |
| IBUPROFEN | ChEMBL | Phase 4 (approved) | PTGS2 |
| ICOSAPENT ETHYL | ChEMBL | Phase 4 (approved) | PTGS2 |
| INDAPAMIDE | ChEMBL | Phase 4 (approved) | PTGS2 |
| INDOCYANINE GREEN ACID FORM | ChEMBL | Phase 4 (approved) | PTGS2 |
| INDOMETHACIN | ChEMBL | Phase 4 (approved) | PTGS2 |
| IPRONIAZID | ChEMBL | Phase 4 (approved) | PTGS2 |
Related Atlas pages
- Genes: PTGS2
- Diseases: rheumatic disorder
- Drugs: Fidaxomicin, 3,3’,4’,5-TETRACHLOROSALICYLANILIDE, Abemaciclib, Acalabrutinib, Acemetacin, Acetophenazine, Acetylcysteine, Acrivastine, Amodiaquine, Amphotericin B, Amsacrine, Anisindione, Apomorphine, Arformoterol, Aspirin, Bazedoxifene, Benzquinamide, Bepridil, Biperiden, Bromfenac, Calcipotriene, Calcitriol, Candesartan Cilexetil, Cannabidiol, Capsaicin, Captopril, Carprofen, Cefazolin, Ceftizoxime, Celecoxib, Cephradine, Cianidanol, Clotrimazole, Crizotinib, Daunorubicin, Deserpidine, Dexibuprofen, Dexketoprofen, Diclofenac, Diethylstilbestrol, Dobutamine, Doxorubicin, Epinephrine, Ergotamine, Esflurbiprofen, Etodolac, Etoricoxib, Flupirtine, Flurbiprofen, Fluvastatin, Folic Acid, Glafenine, Haloperidol, Hexachlorophene, Ibuprofen, Icosapent Ethyl, Indapamide, Indocyanine Green Acid Form, Indomethacin, Iproniazid